Medical and Medicinal Journal

Abstract

Pregnane X receptor (PXR) is a nuclear receptor that exists in forms such as PXR1 and PXR2. Activated PXR1 #heterodimerizes with #retinoid Xreceptor to increase the transcription of #cytochrome P450 3A (CYP3A), a drug-metabolizing enzyme, by binding to the PXR biding site in nuclei. PXR2 is a splice variant of PXR1, which is localized to the nuclei and down regulates the #transcription of CYP3A by PXR1. The present study investigated the roles of PXR1 and PXR2 in the regulation of CYP3A11 expression in adult mouse organs and primary cultured hepatocytes. In the liver and small intestine, which show high expression of CYP3A11 mRNA, PXR1 mRNA was highly expressed while PXR2 mRNA expression was low. In the lung, kidneys, heart, and stomach, which show low expression of CYP3A11 mRNA, both PXR1 and PXR2 mRNA were expressed at high levels.

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Roles of the Nuclear Receptors PXR1 and PXR2 in the Regulation of Cytochrome P450 3A11 Expression in Mouse Organs and Primary-Cultured Hepatocytes by Wataru Ochiai in BJSTR